Table I.

Summary of preclinical tools and clinical therapeutic drugs targeting different process of glutamine metabolism.

First author/s, year	Class	Drug	Mechanism	Stage	Target	(Refs.)
Magill et al, 1957	Glutamine analogue	DON	Widely inhibit the glutamine metabolic enzyme	Limited due to toxicity	Enzyme used by glutamine	(75)
Leone et al, 2019		JHU083	Pro-drug of DON	Preclinical compound tool		(65)
Robinson et al, 2007	GLS inhibitors	BPTES	Inhibition of GLS	Preclinical tool	GLS	(78)
Gross et al, 2014		CB-839		Phase I and II		(80)
Caiola et al, 2020	Transaminase inhibitors	L-cycloserine	Inhibition of TCA cycle	Preclinical tool	GPT2	(61)
Moreadith and Lehninger, 1984		AOA	anaplerosis	Preclinical tool	Aminobutyrate aminotransferase	(96)
Hassanein et al, 2013	Glutamine transporters inhibitors	GPNA	Inhibition of glutamine transport	Preclinical tool	SLC1A5 (also known as ASCT2)	(69)
Wise and Thompson, 2010		BCH	Inhibition of essential amino acids	Preclinical tool	SLC7A5 (also known as LAT1)	(71)
Hu et al, 2020		Sulfasalazine	Inhibition of cysteine-glutamine transport	Phase II for breast cancer	SLC7A11 (also known as xCT)	(73)

AOA, aminooxyacetate; ASCT2, amino acid transporter 2; BCH, 2-aminobicyclo-(2,2,1)-heptane-2-carboxylic acid; BPTES, Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide; DON, 6-Diazo-5-oxo-L-norleucine; GLS, glutaminase; GPNA, L-γ-glutamyl-p-nitroanilide; GPT2, glutamic-pyruvic transaminase 2; LAT1, L-type amino acid transporter; SLC(X)A(Y), solute carrier family (X) member (Y); TCA, tricarboxylic acid.